Jana, Amit Kumar; Singh, Jyotsana; Ganesher, Asha; Kumar, Amit; Banerjee, Arpita; Kumar, Deepak; Verma, Sarvesh Kumar; Sharma, Ashok Kumar; Bhatta, Rabi Sankar; Konwar, Rituraj; Panda, Gautam published the artcile< Tyrosine-Derived Novel Benzoxazine Active in a Rat Syngenic Mammary Tumor Model of Breast Cancer>, Reference of 81107-97-3, the main research area is benzoxazine derivative anticancer breast cancer apoptosis.
In continuing efforts of improving benzoxazepine derivatives as an anti-breast cancer agent, a new chem. entity, benzoxazine, was designed from scaffold morphing. Structure-activity relationship studies revealed that H, -OMe, -CF3, and -F were well tolerated on R1 and R2 positions of ring A, and R2 as -CH2CH2N(CH2)4 (N-Et pyrrolidine) and -CH2CH2N(CH2)5 (N-Et piperidine) chains on ring D increased activities (Series B, Figure 3). 13d selected as a lead compound (IC50: 0.20 to 0.65 μM) induces apoptosis, cell cycle arrest, and loss of mitochondrial membrane potential in breast cancer cells. Compound 13d was formulated into 13d-f using cyclodextrin to improve its solubility for a pharmacokinetic, in vivo efficacy study. Both 13d and 13d-f regressed tumor growth at concentrations of 5 and 20 mg/kg better than tamoxifen without any mortality in a rat syngenic mammary tumor model. Collectively, our data suggest that tyrosine-derived novel benzoxazine 13d could be a potential lead for the treatment of breast cancer and hence deserve further in-depth studies.
Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 81107-97-3 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3O, Reference of 81107-97-3.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary