Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 155559-81-2, Name is 5-Fluorobenzo[d]thiazole-2-thiol, category: thiazole.
As an FDA-approved drug, teniposide, was utilized in cancer treatment but was accompanied by a strong side effect in long-term clinical trials. This work discovered potential candidate drugs with low toxicity by modifying the molecule structure of teniposide through a structure-guided drug design approach. The IC50 value of novel 4,6-O-thenylidene-beta-d-glucopyranoside-(2?-acetamido, 3?-acetyl-di-S-5-fluorobenzothizole/5-fluorobenzoxazole)-4?-demethylepipodophyllotoxin (compounds 15 and 16) was 120.4-125.1 muM, which was significantly improved by around 10 times more than teniposide (11.5-22.3 muM) against healthy human cells (i.e., HL-7702, H8, MRC-5, and HMEC). In vivo studies demonstrated compounds 15 and 16 significantly suppressed the tumor growth in the HepG2 cell xenograft model without exhibiting obvious toxicity (LD50 values of 208.45 and 167.52 mg/kg), which was lower than that of teniposide (LD50 = 46.12 mg/kg). Compounds 15 and 16 caused mild gammaH2AX phosphorylation for low DNA toxicity and less inhibition of PI3K/Akt. Compounds 15 and 16 might be potential antitumor drugs with low toxicity.
Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.category: thiazole. In my other articles, you can also check out more blogs about 155559-81-2
Reference：
Thiazole | C3H6389NS – PubChem,
Thiazole | chemical compound | Britannica