Zenglu Liu

NOVEL SYNTHESIS OF 4- OR 6-SUBSTITUTED INDIRUBIN DERIVATIVES

A simple and convenient route for synthesis of a series of 4- or 6-substituted indirubin derivatives by oxidation and subsequent condensation of indoxyl and isatin is described. Acidic reaction conditions are crucial to the condensation of 4-substituted derivatives, whereas for the condensation of 6-substituted derivatives, both acidic and basic conditions work well.

Convenient Synthesis of Aryl Ferrocenyl Ketone via Palladium‐Catalyzed Carbonylation Coupling

Abstract A series of aryl ferrocenyl ketones were prepared from iodoferrocene, phenylboronic acids, and CO via palladium‐catalyzed carbonylation coupling in a short time. The procedure was efficient and convenient and avoided formation of diacylated derivatives compared with currently available Friedel–Crafts acylation methodologies.

SYNTHESIS OF PYRROLO[2,3-d]PYRIMIDINE ANALOGUES OF THE POTENT ANTITUMOR AGENT N-{4-[3-(2,4-DIAMINO-7H-PYRROLO-[2,3-d]PYRIMIDIN-5-YL)PROPYL]BENZOYL}-L-GLUTAMIC ACID (TNP-351)

Two three-atom-bridged analogues of TNP-351, N-(4-{[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-ylmethyl)amino]methyl}-benzoyl)-L-glutamic acid (4) and N-(4-{[(2,4-diamino-7H-pyrrolo[2,3-d]-pyrimidin-5-ylmethyl)amino]methyl}benzoyl)-L-glutamic acid (5) were synthesized as anticancer agents, and their biological activities were evaluated.

Synthesis and Biological Evaluation of 3-Substituted-4-(4-methylthio phenyl)-1HPyrrole Derivatives as Potential Anticancer Agents

A novel series of 3-substituted-4-(4-methylthio phenyl)-1H-pyrrole derivatives were synthesized via Van Leusen pyrrole synthesis. The in vitro anticancer activity against a panel of 16 cancer cell lines and 2 normal cell lines was investigated by MTT assay. It was found that some of the pyrrole compounds showed similar antiproliferative activity against cancer cells compared with Paclitaxel, but little impact on normal cell lines, which indicated that the novel pyrrole derivatives could be used as potential anticancer candidates for possessing both selectivity and good therapeutic efficacy. Structure-activity relationship analysis found that 3-phenylacetyl-4- (4-methylthio phenyl)-1H-pyrrole derivatives displayed the most strong anticancer activity, among which [4-(4-methylthio phenyl)-1Hpyrrol- 3-yl] (4-methoxy phenyl) methanone (3j) was employed to investigate the effect of these pyrrole analogues on cell cycle by propidium iodide (PI) staining on cell flow cytometry. Cell necrotic effect of 10.0 µM 3j against MGC80-3 cells were also observed under fluorescence microscope and transmission electron microscope by ultrathin sections observation.

Novel Synthesis of Aza-phthalimidine Hydroxylactams

Abstract A novel and convenient synthetic route for preparing aza-phthalimidine hydroxylactams (5a–j) by N-bromosuccinimide (NBS) was developed. This method involved the substitution reactions of substrates (3a–j) with NBS via unstable intermediate bromides (4a–j) rapidly hydrolyzed into hydroxyl products in the course of the workup process.