Zeng, Yanqun published the artcileDesign and synthesis of piperidine derivatives as novel human heat shock protein 70 inhibitors for the treatment of drug-resistant tumors, Recommanded Product: 2-(Chloromethyl)benzonitrile, the publication is European Journal of Medicinal Chemistry (2015), 19-31, database is CAplus and MEDLINE.
HSP70 is a potential target for tumor treatment. HSP70 plays significant roles in several biol. processes, including the regulation of apoptosis. In this study, piperidine derivatives were designed as novel HSP70 inhibitors based on virtual fragment screening performed in Dock 4.0, Discovery Studio 2.5 and SYBYL 6.9. A total of 67 novel piperidine derivatives were synthesized. Cell viability assays were performed in 16 cancer cell lines. The emphasis was placed on lapatinib-resistant breast cancer cells (BT/LapR1.0, MDA-MB-361, SK/LapR1.0, and MDA-MB-453). The compounds I [R = 4-NCC6H4, 2-Cl-4-FC6H3, 2,4-Cl2C6H3, 4-MeC6H4, 2-ClC6H4] significantly inhibited the proliferation of human breast cancer cells. Compound I [R = 4-NCC6H4] (II) inhibited the growth of BT474 and BT/LapR1.0 cells with IC50 values of 1.41 μM and 1.47 μM, resp. The binding affinity of II/HSP70 was evaluated by surface plasmon resonance and yielded Kd values of 2.46 μM. The LD50 was 869.0 mgkg-1. These data suggest that II may be a potential candidate compound for tumor treatment.
European Journal of Medicinal Chemistry published new progress about 612-13-5. 612-13-5 belongs to nitriles-buliding-blocks, auxiliary class Organic Pigment, name is 2-(Chloromethyl)benzonitrile, and the molecular formula is C8H7NaO4S, Recommanded Product: 2-(Chloromethyl)benzonitrile.
Referemce:
https://en.wikipedia.org/wiki/Nitrile,
Nitriles – Chemistry LibreTexts