Hazhmat Ali

Characterization of the Antiproliferative and Antimetastatic Properties of Centrapalus pauciflorus Meroterpenoid Centrapalus Coumarin F

The current study examined the in vitro antineoplastic potentials of centrapalus coumarin F (CCF) obtained from aerial parts of Centrapalus pauciflorus (Willd.) H.Rob. (Asteraceae). Cytotoxic activity was tested against a panel of human adherent cancer cell lines, including breast, cervical, and oropharyngeal cancer and glioblastoma. Cell cycle analyses using flow cytometry and Hoechst 33258-propidium iodide (HOPI) fluorescent double staining were used to describe the proapoptotic property of CCF. Wound healing assessment and the Boyden chamber assay were performed to characterize the antimetastatic action of the compound. The firefly luciferase assay was applied to clarify the action of CCF on estrogenic receptors. CCF demonstrated remarkable selective growth inhibition against the HPV-18-positive human cervical cancer cell line HeLa (IC50 = 2.28 µM). The compound elicited crucial markers of apoptosis, inhibited the migration and invasion capacity of HeLa cells, and demonstrated an antiestrogenic property. Our current data indicate that the meroterpenoid scaffold presented here displays remarkable antiproliferative and antimetastatic effects on HeLa cells and can be considered a valuable model for designing further analogs targeting cervical carcinoma.

Synthesis and Antiproliferative Activity of Steroidal Diaryl Ethers

Novel 13α-estrone derivatives have been synthesized via direct arylation of the phenolic hydroxy function. Chan–Lam couplings of arylboronic acids with 13α-estrone as a nucleophilic partner were carried out under copper catalysis. The antiproliferative activities of the newly synthesized diaryl ethers against a panel of human cancer cell lines (A2780, MCF-7, MDA-MB 231, HeLa, SiHa) were investigated by means of MTT assays. The quinoline derivative displayed substantial antiproliferative activity against MCF-7 and HeLa cell lines with low micromolar IC50 values. Disturbance of tubulin polymerization has been confirmed by microplate-based photometric assay. Computational calculations reveal significant interactions of the quinoline derivative with the taxoid binding site of tubulin.