Temburnikar, Kartik W.; Ross, Christina R.; Wilson, Gerald M.; Balzarini, Jan; Cawrse, Brian M.; Seley-Radtke, Katherine L. published the artcile< Antiproliferative activities of halogenated pyrrolo[3,2-d]pyrimidines>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is halogenated pyrrolo pyrimidine derivative preparation antitumor cancer; Apoptosis; Cell cycle arrest; Cytostatic; Heterocyclic chemistry; Thieno[3,2-d]pyrimidine.
In vitro evaluation of the halogenated pyrrolo[3,2-d]pyrimidines identified antiproliferative activities in compounds 1 and 2 against four different cancer cell lines. Upon screening of a series of pyrrolo[3,2-d]pyrimidines, the 2,4-Cl compound 1 was found to exhibit antiproliferative activity at low micromolar concentrations Introduction of iodine at C7 resulted in significant enhancement of potency by reducing the IC50 into sub-micromolar levels, thereby suggesting the importance of a halogen at C7. This finding was further supported by an increased antiproliferative effect for 4 as compared to 3. Cell-cycle and apoptosis studies conducted on the two potent compounds 1 and 2 showed differences in their cytotoxic mechanisms in triple neg. breast cancer MDA-MB-231 cells, wherein compound 1 induced cells to accumulate at the G2/M stage with little evidence of apoptotic death. In contrast, compound 2 robustly induced apoptosis with concomitant G2/M cell cycle arrest in this cell model.
Bioorganic & Medicinal Chemistry published new progress about Antiproliferative agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
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