152586-91-9Relevant academic research and scientific papers
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
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
2-PHENYL BENZOTHIAZOLE LINKED IMIDAZOLE COMPOUNDS AS POTENTIAL ANTICANCER AGENTS AND PROCESS FOR THE PREPARATION THEREOF
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Page/Page column 19-21, (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.
Antitumor benzothiazoles. 3. Synthesis of 2-(4- aminophenyl)benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo
Shi, Dong-Fang,Bradshaw, Tracey D.,Wrigley, Samantha,McCall, Carol J.,Lelieveld, Peter,Fichtner, Iduna,Stevens, Malcolm F. G.
, p. 3375 - 3384 (2007/10/03)
A new series of 2-(4-aminophenyl)benzothiazoles substituted in the phenyl ring and benzothiazole moiety has been synthesized by simple, high- yielding routes. The parent molecule 5a shows potent inhibitory activity in vitro in the nanomolar range against a panel of human breast cancer cell lines, but is inactive (IC50 > 30 μM) against other cell types: activity against the sensitive breast lines MCF-7 and MDA 468 is characterized by a biphasic dose-response relationship. Structure-activity relationships derived using these cell types has revealed that activity follows the heterocyclic sequence benzothiazole > benzoxazole >> benzimidazole and that 2-(4-aminophenyl)benzothiazoles bearing a 3'-methyl- 9a, 3'-bromo- 9c, 3'- iodo- 9f, and 3'-chloro-substituent 9i are especially potent and their activity extends to ovarian, lung, and renal cell lines. Four compounds have been evaluated in vivo against human mammary carcinoma models in nude mice. Compound 9a showed the most potent growth inhibition against the ER+ (MCF- 7 and BO) and ER- (MT-1 and MT-3) tumors. Our efforts to identify a pharmacological mechanism of action for these intriguing compounds have not, as yet, been successful.
