Synthesis, biological evaluation and molecular docking studies of new pyrazolines as an antitubercular and cytotoxic agents.

Synthesis, biological evaluation and molecular docking studies of new pyrazolines as an antitubercular and cytotoxic agents. Infect Disord Drug Targets. 2018 Dec 17;: Authors: Lokesh BVS, Prasad YR, Shaik AB Abstract A series of new pyrazolines containing 2,5-dichloro-3-acetylthiophene chalcone moiety (PZT1-PZT20) have been synthesized, characterized by 1HNMR and 13CNMR and evaluated for them in vitro antitubercular activity against M. tuberculosis H37Rv strain and in vitro anticancer activity against DU-145 prostate cancer cell lines. Majority of screened compounds have displayed potential activity against Mycobacterium tuberculosis H37Rv(MTB) strain and anticancer activity against DU-149 prostate cancer cell lines. Among the series, compound PZT5 with 2", 4"-dichlorophenyl group at 5-position on the pyrazoline ring exhibited the most potent antitubercular activity (MIC=1.60 µg/mL) and compounds PZT2, PZT9, PZT11, PZT15, and PZT20 showed similar antitubercular activity against standard pyrazinamide (MIC=3.12 µg/mL) by broth dilution assay.. PZT15 and PZT17 with 4"-pyridinyl and 2"-pyrrolyl groups on pyrazoline ring were found to exhibit better anticancer activity against DU-149 prostate cancer cell lines with IC50 values of 2.0±0.2 µg/mL and 6.0±0.3 µg/mL respectively by MTT assay. The preliminary structure-activity relationship has been summarized. The molecular docking studies with crystalline structures of enoyl acyl carrie...
Source: Infectious Disorders Drug Targets - Category: Infectious Diseases Authors: Tags: Infect Disord Drug Targets Source Type: research