1393816-22-2Relevant academic research and scientific papers
2-Arylaminobenzothiazole-arylpropenone conjugates as tubulin polymerization inhibitors
Subba Rao,Rao, Bala Bhaskara,Sunkari, Satish,Shaik, Siddiq Pasha,Shaik, Bajee,Kamal, Ahmed
, p. 924 - 941 (2017/07/12)
A new series of 2-arylaminobenzothiazole-arylpropenone conjugates 5-6(a-r) was designed, synthesized and investigated for their cytotoxic potency against the various human cancer cell lines. Most of these conjugates exhibited cytotoxic activity and inhibi
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers
Subba Rao,Swapna, Konderu,Shaik, Siddiq Pasha,Lakshma Nayak,Srinivasa Reddy,Sunkari, Satish,Shaik, Thokhir Basha,Bagul, Chandrakant,Kamal, Ahmed
, p. 977 - 999 (2017/02/05)
A series of colchicine site binding tubulin inhibitors were synthesized by the modification of the combretastatin pharmacophore. The ring B was replaced by the pharmacologically relevant benzothiazole scaffolds, and the cis configuration of the olefinic b
Synthesis and study of benzothiazole conjugates in the control of cell proliferation by modulating Ras/MEK/ERK-dependent pathway in MCF-7 cells
Kamal, Ahmed,Faazil, Shaikh,Ramaiah, M. Janaki,Ashraf, Md.,Balakrishna,Pushpavalli,Patel, Nibedita,Pal-Bhadra, Manika
supporting information, p. 5733 - 5739 (2013/10/01)
By applying a methodology, a series of benzothiazole-pyrrole based conjugates (4a-r) were synthesized and evaluated for their antiproliferative activity. Compounds such as 4a, 4c, 4e, 4g-j, 4m, 4n, 4o and 4r exhibited significant cytotoxic effect in the MCF-7 cell line. Cell cycle effects were examined for these conjugates at 2 μM as well as 4 μM concentrations and FACS analysis show an increase of G2/M phase cells with concomitant decrease of G1 phase cells thereby indicating G2/M cell cycle arrest by them. Interestingly 4o and 4r are effective in causing apoptosis in MCF-7 cells. Moreover, 4o showed down regulation of oncogenic expression of Ras and its downstream effector molecules such as MEK1, ERK1/2, p38 MAPK and VEGF. The apoptotic aspect of this conjugate is further evidenced by increased expression of caspase-9 in MCF-7 cells. Hence these small molecules have the potential to control both the cell proliferation as well as the invasion process in the highly malignant breast cancers.
2-PHENYL BENZOTHIAZOLE LINKED IMIDAZOLE COMPOUNDS AS POTENTIAL ANTICANCER AGENTS AND PROCESS FOR THE PREPARATION THEREOF
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Page/Page column 22-25, (2012/09/10)
The present invention provides 2-phenyl benzothiazole linked imidazole compounds of formula A as anti cancer agent against fifty three human cancer cell lines. (General formula A) wherein (II) R=H or OCH3; R1=H, F or OCH3; R2=H or OCH3; R3=H, NH2, F or OCH3; R4=H, NH2 or OCH3; R5=H, NH2, F, CF3 or OCH3; R6=H or OCH3; R7=H or OCH3; R8=H or OCH3.
