39500-10-2Relevant academic research and scientific papers
Design and synthesis of β-carboline and combretastatin derivatives as anti-neutrophilic inflammatory agents
Kumar, Sunil,Wang, Yi-Hsuan,Chen, Po-Jen,Chang, Yu-Chia,Kashyap, Hemant K.,Shen, Ya-Ching,Yu, Huang-Ping,Hwang, Tsong-Long
, (2021)
A series of β-carboline derivatives was synthesized by the Pictet-Spengler reaction with or without the combretastatin skeleton. The structures of these derivatives were elucidated by spectroscopic techniques. All synthesized compounds were evaluated for
Synthesis and in vitro cytotoxicity evaluation of β-carboline-combretastatin carboxamides as apoptosis inducing agents: DNA intercalation and topoisomerase-II inhibition
Jadala, Chetna,Sathish,Reddy, T. Srinivasa,Reddy, Velma Ganga,Tokala,Bhargava, Suresh K.,Shankaraiah, Nagula,Nagesh, Narayana,Kamal
, p. 3285 - 3298 (2019/06/20)
To explore a new set of cytotoxic agents, β-carboline-combretastatin carboxamide conjugates were designed, synthesized and evaluated for their in vitro cytotoxicity potential, DNA binding affinity and Topoisomerase-II (topo-II) inhibition activity. Among the designed hybrids, 10v and 10af have shown significant cytotoxic effect against A549 (lung cancer) cell line having IC50 value 1.01 μM and 1.17 μM respectively. Further, it was speculated that treatment with compound 10v may induce apoptosis among A549 cells, which was supported by Hoechst staining, DCFDA, Annexin V-FITC and morphological assays. Flow cytometric analysis revealed that the hybrid 10v arrests A549 cells in G2/M phase of cell cycle in a dose dependent manner. Amongst the active hybrids, most potent hybrid 10v was tested for DNA topo-II inhibition activity. Moreover, to further support the biological activity and to infer the mode of interaction between ligands and DNA, spectroscopy and molecular docking studies were carried out. The docking and spectroscopy results showed that the ligands exhibited an intercalative mode of binding with DNA and could efficiently bind to DNA and form topo-II ternary complex. Based on these experiments, the hybrids 10v and 10af were identified as proficient new scaffolds which need to be developed as hit molecules for therapeutic interest.
Synthesis and biological evaluation of 4β-acrylamidopodophyllotoxin congeners as DNA damaging agents
Kamal, Ahmed,Suresh, Paidakula,Janaki Ramaiah,Mallareddy, Adla,Kumar, Banala Ashwini,Raju, Paidakula,Vinay Gopal,Pushpavalli,Lavanya,Sarma, Pranjal,Pal-Bhadra, Manika
experimental part, p. 4589 - 4600 (2011/09/19)
A series of new 4β-acrylamidopodophyllotoxin derivatives (13a-o) were synthesized by coupling of substituted acrylic acids (10a-l and 11m-o) to the 4β-aminopodophyllotoxin. The synthesized derivatives 13a-o were evaluated for their cytotoxicity against fi
COMBRETASTATIN DERIVATIVES AND RELATED THERAPEUTIC METHODS
-
Page/Page column 27-28; 49, (2008/06/13)
Compounds of the formula (I) wherein R1, R5, R6, R7 and R10 are H, wherein R2, R3, R4 and R8 are OMe, and wherein R9 is -X-CO-R", R" is an unsubstituted or a substituted alkyl, alkenyl or aryl group comprising 5-21 carbon atoms and does not include N, and X is O, S or N, compounds related thereto, and methods for their use, particularly for modulating tumor growth or metastasis in an animal.
