Tail-approach based design, synthesis, and cytotoxic evaluation of novel disubstituted and trisubstituted 1,3-thiazole benzenesulfonamide derivatives with suggested carbonic anhydrase IX inhibition mechanism

Abstract

A novel series of 2,4,5- and 2,3,4-trisubstituted thiazole hybrids with 1,3,4-thiadiazolylbenzenesulfonamide was designed following the tail approach as possible hCAIX inhibitors.

Design, synthesis, and anticancer evaluation of novel coumarin/thiazole congeners as potential CDK2 inhibitors with molecular dynamics

“…hy926 as a normal human cell line was used for evaluation using sulforhodamine B (SRB) assay. 48–51 The cell lines were purchased from ATCC and cultured in RPMI-1640 with penicillin (100 U mL −1 )–streptomycin (100 μg mL −1 ) and heat-inactivated fetal bovine serum (10% v/v) at 37 °C and 5% (v/v) CO 2 . The growing cells were trypsinized and cultured in a 96-well tissue culture plate for 24 h before being manipulated.…”

Computational insights into novel benzenesulfonamide-1,3,4-thiadiazole hybrids as a possible VEGFR-2 inhibitor: design, synthesis and anticancer evaluation with molecular dynamics studies

“…At a wavelength of 570 nm, the absorbance of the resulting mixture was measured against the medium as blank for each measurement. 54–56…”

New edaravone analogs incorporated with N‐benzylthiazole moiety: Multistep chemical synthesis, in vitro cytotoxicity with pRIPK3 inhibitory activities, and molecular docking

“…Afterward, we focused on the thiazolation of benzyllthiosemicarbazone 2 by reaction first with commercially available bifunctional α-chlorinated compounds (chloroacetyl chloride or ethyl chloroacetate) as useful building blocks in refluxing dioxane containing a catalytic amount of anhydrous sodium acetate [27] to install the corresponding N-benzyl-4-thiazolone derivative 3 in high yield (Scheme 2). The generation of 3 was conducted via the heterocyclization process [28,29]. The aliphatic and aromatic regions of 3 are clearly distinguished in the 1D NMR spectra.…”