Byrappa, Sathish; Rachaiah, Kavitha; Kotian, Sumana Y.; Balaraju, Yashaswini; Prabhuswamimath, Samudyata C.; Rai, Kuriya M. L.; Salimath, Bharathi P. published the artcile< Synthesis and Screening of Pro-apoptotic and Angio-inhibitory Activity of Novel Benzisoxazole Derivatives both In Vitro and In Vivo>, Reference of 84163-77-9, the main research area is phenyl dihydroisoxazolyl methylpiperidinyl fluorobenzoisoxazole preparation; antitumor antiangiogenic activity retinal neovascularization apoptosis; Benzisoxazole; anti-angiogenesis; anti-cancer; antiproliferative; apoptosis; breast cancer; cytotoxicity; piperidine..
Novel derivatives of Benzisoxazoles I [R1 = H, MeO, BnO; R2 = H, F, MeO, Cl, BnO; R3 = H, MeO] were synthesized and screened for their biol. potential. Chem. synthesis, Mass spectrometry (HRMS), cell proliferation and cytotoxicity assay, wound healing assay, flow cytometry and nuclear staining were reported. Angio-inhibitory activity assessed by corneal micropocket assay and in-vivo peritoneal angiogenesis assay. Compounds I were synthesized and screened for their biol. potency by both in-vitro and in-vivo exptl. models. Among the series, compound I [R1 = BnO, R2 = MeO, R3 = H] was found to be most promising, with an average IC50 value of 50.36 ± 1.7 μM in MTT assay and showed 81.3% cell death. The compound I [R1 = BnO, R2 = MeO, R3 = H] also showed 60-70% inhibition on a recombinant Metastasis-Associated protein (MTA1) induced proliferation and cell migration in MDAMB-231 cells, which is known to play a major role in angiogenesis. The anti-tumor studies inferred the regression of tumor activity. This was due to inhibition of neovascularization and evoking apoptosis process as assessed by corneal vascularization, peritoneal angiogenesis and apoptotic hallmarks in compound I [R1 = BnO, R2 = MeO, R3 = H] treated cells. These findings not only showed the biol. efficacy of compound I [R1 = BnO, R2 = MeO, R3 = H] but it was also an effective beginning to explore the mechanism of metastasis and cancer therapy strategy targeting MTA1. The observed biol. activity made compound I [R1 = BnO, R2 = MeO, R3 = H] an attractive drug candidate.
Anti-Cancer Agents in Medicinal Chemistry published new progress about Angiogenesis. 84163-77-9 belongs to class benzisoxazole, and the molecular formula is C12H13FN2O, Reference of 84163-77-9.
Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics