Synthesis of new thienylpicolinamidine derivatives and possible mechanisms of antiproliferative activity.

ABSTRACT: Three thienylpicolinamidine derivatives 4a-c were prepared from their corresponding picolinonitriles 3a-c on treatment with lithium trimethylsilylamide, LiN(TMS)₂, followed by a de-protection step using ethanol/HCl (gas). DFT calculations were used to optimize the geometric structure of the newly synthesized picolinamidines. The comparison of DFT calculated spectral data with the experimental data (¹H-NMR and ¹³C-NMR) showed a good agreement. The in vitro antiproliferative activity of the cationic compounds 4a-c was determined against 60 cancer cell lines representing nine types of cancer. The tested picolinamidines were highly active with compounds 4a and 4b eliciting mainly cytotoxic activity with GI values ranging from -7.17 to -86.03. Leukemia (S

SUBMITTER: Ismail MA 

PROVIDER: S-EPMC9057764 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature