Use of Parthenolide Derivatives as Antileukemic and Cytotoxic Agents

Melampomagnolide B Derivatives as Antileukemic and Cytotoxic Agents

Synthesis and Biological Evaluation of 2-Phenyl Benzothiazole Derivatives as Cytotoxic Agents

Cancer is a leading cause of death worldwide. Many heterocyclic cores are present in the structures of clinically approved anticancer drugs. Meanwhile, benzothiazoles have been reported as one of the most important heterocyclic scaffolds in previously reported anticancer agents in the literature. Therefore, in this report, a novel series of 2-phenyl benzothiazole derivatives was synthesized, bi...

Chemoenzymatic synthesis and antileukemic activity of novel C9- and C14-functionalized parthenolide analogs.

Parthenolide is a naturally occurring terpene with promising anticancer properties, particularly in the context of acute myeloid leukemia (AML). Optimization of this natural product has been challenged by limited opportunities for the late-stage functionalization of this molecule without affecting the pharmacologically important α-methylene-γ-lactone moiety. Here, we report the further developm...

Design and Synthesis of Pyrrolo[2,1-a]Isoquinoline-Based Derivatives as New Cytotoxic Agents

A new series of anti-cancer agents based on 1,2-diaryl-5,6-dihydropyrrolo[2,1-a]isoquinoline scaffold containing N,N-diethylamino‌ethoxy, piperidinyl‌ethoxy or morpholinyl‌ethoxy group at the para position of the C-2 phenyl ring were synthesized and their cytotoxic activities were assessed against several human cancer cell lines including MCF-7 (ER positive breast cancer cell), MDA-MB231 (ER-ne...

Synthesis, Biological Evaluation and Docking Analysis of Some Novel Quinazolin Derivatives as Antitumor Agents

Different acid chlorides (2a-d) reacted with anthranilic acid to produce 2-substituted-3, 1-benzoxazin-4-one (3a-d) which was used as starting material to synthesize some condensed and non-condensed heterocyclic compounds by reaction with nitrogen nucleophiles e.g., hydrazine hydrate, and formamide. Some of the newly synthesized analogues were chosen to evaluate their cytotoxic activity against...