Xie, Lan published the artcileLead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents, Application In Synthesis of 73874-95-0, the main research area is phenanthrene tylophorine preparation antitumor activity SAR.
Phenanthrene-based tylophorine-1 (PBT-1) I (R = CH2OH, NHBoc, Me, SO2Me, etc.; R1 = H, OMe; R2 = OH, OMe, OAc, prop-2-yn-1-yloxidanyl, etc.; X = CH, N) and II (R3 = H, OMe; R4 = H, OMe) was identified previously as a lead compound in an anticancer drug discovery effort based on natural Tylophora alkaloids. An expanded structural optimization using a new more efficient synthetic route provided 14 PBT-derivatives I and II. Eleven compounds displayed obvious antiproliferative activities in cellular assays (GI50 0.55-9.32μM). The most potent compounds I (R = CH2OH, R1 = H, R2 = OH, X = CH; R = NHBoc, R1 = H, R2 = OH, X = CH; R = NH2, R1 = H, R2 = OH, X = CH) (GI50 ; 1μM) contained a 7-hydroxy group on the phenanthrene B-ring in addition to a pendant piperidine E-ring with different 4-substituents. While I (R = NH2, R1 = H, R2 = OH, X = CH) with NH2 as the piperidine substituent was at least 4-fold more potent against triple-neg. breast cancer MDA-MB-231 than estrogen-responsible breast cancer MCF-7 cell growth. In further biol. evaluations, the new active compounds induced cell cycle accumulation in late S and G2/M phase without interfering with microtubule formation or cell morphol. These results on the optimization of the B- and E-rings of PBT-1 I and II should benefit the further development of novel antitumor agents.
ACS Medicinal Chemistry Letters published new progress about Alkaloids Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Application In Synthesis of 73874-95-0.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem