- Synthesis, DNA binding ability and anticancer activity of 2-heteroaryl substituted benzimidazoles linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates
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As a continuation of our efforts to develop the benzimidazole-PBD conjugates as potential anticancer agents, a series of heteroaryl substituted benzimidazole linked PBD conjugates has been synthesized and evaluated for their anticancer potential in 60 human cancer cell lines. Most of the compounds exhibited promising anticancer activity and interestingly, compounds 4c and 4d displayed significant activity in most of the cell lines tested. Whereas, compound 4e showed selectivity in renal cancer cells with GI50 values of 10 and 70 nM against RXF 393 and UO-31 cell lines, respectively. Further, these compounds also showed significant DNA-binding affinity by thermal denaturation study using duplex form of calf thymus (CT) DNA.
- Kamal, Ahmed,Pogula, Praveen Kumar,Khan, Mohammed Naseer Ahmed,Seshadri, Bobburi Naga,Sreekanth, Kokkonda
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p. 651 - 659
(2013/09/23)
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- Synthesis of benzopyran linked pyrrolo[2,1-c][1,4]benzodiazepines as DNA-binding and potential anticancer agents
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A series of twelve benzopyran linked pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) have been synthesized. They exhibit significant DNA-binding activity and excellent cytotoxic activity against various human cancer cell lines.
- Kamal, Ahmed,Rajender,Reddy, Methuku Kashi,Reddy, Vangala Santhosh,Kumar, Gajjela Bharath
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p. 177 - 192
(2013/07/28)
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- Design, synthesis and biological evaluation of imidazo[1,5-a]pyridine-PBD conjugates as potential DNA-directed alkylating agents
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A series of novel imidazo[1,5-a]pyridine-PBD conjugates were synthesized and evaluated for their antitumor activity in breast cancer cell line (MCF-7). Interestingly, all the compounds showed enhanced DNA binding ability. These conjugates showed significa
- Kamal, Ahmed,Ramakrishna,Ramaiah, M. Janaki,Viswanath,Rao, A. V. Subba,Bagul, Chandrakant,Mukhopadyay, Debasmitha,Pushpavalli,Pal-Bhadra, Manika
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p. 697 - 703
(2013/06/05)
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- Design and synthesis of benzo[c,d]indolone-pyrrolobenzodiazepine conjugates as potential anticancer agents
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A series of benzo[c,d]indol-2(1H)one-PBD conjugates (11a-l) have been designed and synthesized as potential anticancer agents. These compounds were prepared by linking the C8-position of DC-81 with a benzo[c,d]indol-2(1H)one moiety through different alkane spacers in good yields and confirmed by 1H NMR, mass and HRMS data. The DNA binding ability of these conjugates was evaluated by thermal denaturation studies and interestingly, compound 11l showed enhanced DNA binding ability. These compounds were also evaluated for their anticancer activity in selected human cancer cell lines of lung, skin, colon and prostate by using MTT assay method. These new conjugates showed promising anticancer activity with IC50 values ranging from 1.05 to 36.49 μM. Moreover, cell cycle arrest in SubG1 phase was observed upon treatment of A549 cells with 1 and 2 μM (IC50) concentrations of compound 11l and it induced apoptosis. This is confirmed by Annexin V-FITC, Hoechst staining, caspase-3 activity as well as DNA fragmentation analysis.
- Kamal, Ahmed,Ramakrishna,Lakshma Nayak,Raju,Subba Rao,Viswanath,Vishnuvardhan,Ramakrishna, Sistla,Srinivas
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experimental part
p. 789 - 800
(2012/03/27)
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- Synthesis, DNA binding and anticancer activity of pyridylimidazolidinone linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates
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A series of pyridylimidazolidinone linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates have been synthesized and evaluated for their DNA binding ability and cytotoxicity. These conjugates exhibited significant DNA binding ability and potent anticanc
- Kamal, Ahmed,Kumar, B. Ashwini,Suresh, Paidakula
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experimental part
p. 234 - 241
(2012/05/20)
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- Synthesis and biological evaluation of cinnamido linked pyrrolo[2,1-c][1,4]benzodiazepines as antimitotic agents
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A series of new cinnamido-pyrrolo[2,1-c][1,4]benzodiazepine conjugates (4a-d and 5a-d) and their dimers (6a-d) have been designed, synthesized and evaluated for their biological activity. The anticancer screening of compound 4a by the NCI exhibited signif
- Kamal, Ahmed,Balakishan,Ramakrishna,Basha Shaik,Sreekanth,Balakrishna,Rajender,Dastagiri,Kalivendi, Shasi V.
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experimental part
p. 3870 - 3884
(2010/09/14)
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- Synthesis and potential cytotoxic activity of new phenanthrylphenol-pyrrolobenzodiazepines
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New phenanthrylphenol-pyrrolobenzodiazepine (PP-PBD) conjugates have been synthesized and evaluated for their biological activity. One of the compounds 4a has been evaluated for its antiproliferative activity on 57 human tumour cell lines. The growth inhi
- Kamal, Ahmed,Sreekanth, Kokkonda,Kumar, P. Praveen,Shankaraiah, Nagula,Balakishan,Ramaiah, M. Janaki,Pushpavalli,Ray, Paramita,Bhadra, Manika Pal
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scheme or table
p. 2173 - 2181
(2010/06/17)
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- Synthesis, anticancer activity and apoptosis inducing ability of anthranilamide-PBD conjugates
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A series of novel anthranilamide linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates were prepared and evaluated for their anticancer activity. The effects of three promising PBD conjugates on cell cycle of cancerous cell line A375 were investigated. Thes
- Kamal, Ahmed,Vijaya Bharathi,Janaki Ramaiah,Surendranadha Reddy,Dastagiri,Viswanath,Sultana, Farheen,Pushpavalli,Pal-Bhadra, Manika,Juvekar, Aarti,Sen, Subrata,Zingde, Surekha
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scheme or table
p. 3310 - 3313
(2010/08/19)
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- Phosphonate-linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: Synthesis, DNA-binding affinity and cytotoxicity
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Pyrrolobenzodiazepine-diethylphosphonate conjugates have been designed and synthesized that link through two different types of spacers that are simple alkane chain and also a piperazine moiety side-armed with the alkane chains. These pyrrolobenzodiazepin
- Kamal, Ahmed,Kumar, P. Praveen,Seshadri,Srinivas,Kumar, M. Shiva,Sen, Subrata,Kurian, Nisha,Juvekar, Aarti S.,Zingde, Surekha M.
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p. 3895 - 3906
(2008/12/21)
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- Synthesis of C8-C8/C2-C8-linked triazolo pyrrolobenzodiazepine dimers by employing 'click' chemistry and their DNA-binding affinity
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A series of 1,2,3-triazole-containing pyrrolo[2,1-c][1,4]benzodiazepine dimers have been prepared efficiently by employing a 'click' chemistry protocol. This method involves 1,3-dipolar cycloaddition of terminal alkynes with organic azides using a Cu(I)-c
- Kamal, Ahmed,Prabhakar,Shankaraiah,Reddy, Ch. Ratna,Reddy, P. Venkat
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p. 3620 - 3624
(2008/09/21)
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- Synthesis of new benzimidazole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates with efficient DNA-binding affinity and potent cytotoxicity
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The synthesis of new benzimidazole linked pyrrolobenzodiazepine conjugates is described. Some of these conjugates show significant DNA-binding affinity and, a representative compound 4c shows promising in vitro cytotoxicity against a number of human cance
- Kamal, Ahmed,Praveen Kumar,Sreekanth,Seshadri,Ramulu
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p. 2594 - 2598
(2008/12/21)
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- PYRROLO[2,1-C][1,4]BENZODIAZEPINE-NAPTHALIMIDE CONJUGATES LINKED THROUGH PIPERAZINE MOIETY AND PROCESS FOR PREPARATION THEREOF
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The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety as potential antitumour agents. The present invention also relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]
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Page/Page column 6-7; 8-9
(2008/06/13)
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- DNA binding potential and cytotoxicity of newly designed pyrrolobenzodiazepine dimers linked through a piperazine side-armed-alkane spacer
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New pyrrolobenzodiazepine (PBD) dimers have been developed that are composed of two DC-81 subunits tethered to their C8 positions through piperazine moiety side-armed with alkaneoxy linkers (composed of 2-5 carbons). DNA thermal denaturation studies show
- Kamal, Ahmed,Murali Mohan Reddy,Rajasekhar Reddy,Laxman
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p. 385 - 394
(2007/10/03)
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- Pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide conjugates linked through piperazine moiety and process for preparation thereof
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The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety as potential antitumour agents. The present invention also relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]
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Page/Page column 7; 9
(2008/06/13)
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- Pyrrolo[2,1-c][1,4] benzodiazepines compounds and process thereof
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The present invention provides Analogues of 1,1′-{[(bisalkane-1,N-diyl)piperazine]dioxy}bis(11aS)-7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one] of formula (VI) where n=2 to 10; a pharmaceutical composition comprising the above
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Page/Page column 6
(2008/06/13)
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- PYRROLO[(2,1-C)(1,4) BENZODIAZEPINES DIMERS AS ANTITUMOUR AGENTS AND PROCESS THEREOF
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The present invention provides Analogues of 1, 1'-{[(bisalkane-1,N-diyl)piperazine]dioxy}bis(11aS)-7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one] of formula (VI) where n = 2 to 10; a pharmaceutical composition comprising the abo
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- Synthesis of C-8 alkylamino substituted pyrrolo[2,1-c][1,4]benzodiazepines as potential anti-cancer agents
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The design and facile synthesis of C-8 alkylamino substituted pyrrolo[2,1-c][1,4]benzodiazepines is described. These have been prepared by linking the amines at C-8 position with propane spacer to improve solubility in water, and their in vitro cytotoxici
- Kamal, Ahmed,Laxman,Ramesh,Srinivas,Ramulu
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p. 1917 - 1919
(2007/10/03)
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- Design, synthesis, and evaluation of new noncross-linking pyrrolobenzodiazepine dimers with efficient DNA binding ability and potent antitumor activity
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New sequence selective mixed imine-amide pyrrolobenzodiazepine (PBD) dimers have been developed that are comprised of DC-81 and dilactam of DC-81 subunits tethered to their C8 positions through alkanedioxy linkers (comprised of three to five and eight car
- Kamal, Ahmed,Ramesh,Laxman,Ramulu,Srinivas,Neelima,Kondapi, Anand K.,Sreenu,Nagarajaram
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p. 4679 - 4688
(2007/10/03)
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- Synthesis of novel non-cross-linking pyrrolobenzodiazepines with remarkable DNA binding affinity and potent antitumour activity
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Mixed imine-amide pyrrolobenzodiazepine dimers have been prepared which exhibit potent antitumour activity and have significant DNA binding affinity; one of them, 1c, has been shown to cause a remarkable rise in the melting temperature of calf thymus DNA.
- Kamal,Laxman,Ramesh,Neelima,Kondapi
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p. 437 - 438
(2007/10/03)
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