We recently reported the crystal structure of tubulin in complex with a colchicine binding site
inhibitor (CBSI), ABI-231, having 2-aryl-4-benzoyl-imidazole (ABI). Based on this and …

Based on our prior antitumor hits, 32 novel N-alkyl-N-substituted phenylpyridin-2-amine
derivatives were designed, synthesized and evaluated for cytotoxic activity against A549 …

We report the design, synthesis, and biological evaluation of heterocyclic-fused pyrimidines
as tubulin polymerization inhibitors targeting the colchicine binding site with significantly …

Abstract A series of Pyrazolo [1, 5-a] Pyrimidine analogs were designed and synthesized as
novel tubulin inhibitors. Among them, compounds 1a and 1b showed the highest …

Novel indazole and benzimidazole analogues were designed and synthesized as tubulin
inhibitors with potent antiproliferative activities. Among them, compound 12b exhibited the …

Small molecules that interact with the colchicine binding site in tubulin have demonstrated
therapeutic efficacy in treating cancers. We report the design, syntheses, and antitumor …

Abstract By removing 5-methyl and 6-acetyl groups in our previously reported compound 3,
we designed a series of novel 2, 7-diaryl-[1, 2, 4] triazolo [1, 5-a] pyrimidine derivatives as …

Polymerization of tubulin dimers to form microtubules is one of the key events in cell
proliferation. The inhibition of this event has long been recognized as a potential treatment …

Because of its multifaceted role in cellular functions, tubulin is a validated and productive
drug target for cancer therapy. While many tubulin inhibitors demonstrate clinical efficacy …

Targeting the colchicine binding site on tubulin is a promising strategy to develop cancer
therapeutics. Herein, we describe our systematic structure–activity relationship studies of …