+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Design, synthesis and biological evaluation of novel 3-(2-oxo-2-substituted acetamido)benzamides as PARP-1 inhibitors

, : Design, synthesis and biological evaluation of novel 3-(2-oxo-2-substituted acetamido)benzamides as PARP-1 inhibitors. Yao Xue Xue Bao 50(6): 738-745

Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.


PMID: 26521446

Other references

Dubrovin, I.A.; Likhachev, V.N.; Sorokin, B.S., 1982: Potential for increasing the efficiency of dried skim milk production. Data obtained from dairy factories in RFSSR indicate that of 180 factories producing dried skim milk with an av. output of 390 t/shift, 40% are factories producing only up to 1 t/shift. Only 15.5% were large factories with an av. output exceeding...

Hess, P., 1958: Environmental influences on healing of cervical carcinoma. Strahlentherapie 107(1): 127-132

Nathan, D.G.; Schupak, E.; Stohlman, F.; Merrill, J.P., 1964: Erythropoiesis In Anephric Man. Journal of Clinical Investigation 43: 2158-2165

Hansson, C.; Linder-Aronson, S., 1972: Gingival status after orthodontic treatment of impacted upper canines. Transactions. European Orthodontic Society: 433-441

Eltahir, E.A.B.; Bras, R.L., 1993: On the response of the tropical atmosphere to large-scale deforestation. Recent studies on the Amazon deforestation problem predict that removal of the forest will result in a higher surface temperature, a significant reduction in evaporation and precipitation, and possibly significant changes in the tropical circulati...

Romero, E.; Sobral, J.; Luengo, M.A.; Marzoa, J.A., 2001: Values and antisocial behavior among Spanish adolescents. A number of studies have indicated that delinquent adolescents have characteristic value systems. However, most of these studies have adopted a "known-groups" design--that is, they have compared institutionalized delinquents and non-inst...

Okulewicz, A., 1982: Thomix tridens (Capillariidae, Nematoda) in the nightingale Luscinia megarhynchos (Turdidae) in Poland. Wiadomosci Parazytologiczne 28(3-4): 483-487

Hamon S.; Hamon P., 1991: Future prospects of the genetic integrity of two species of okra abelmoschus esculentus and abelmoschus caillei cultivated in west africa. A study of the geographical distribution of two species of okra, Abelmoschus esculentus and A. caillei, shows that both are cultivated in almost all villages from the Gulf of Guinea to the southern limit of the Sahel. If the cultivars of both spec...

Awada, A.; Biganzoli, L.; Cufer, T.; Beex, L.; Lohrisch, C.; Batter, V.; Hamilton, A.; Nooij, M.; Piccart, M., 2002: An EORTC-IDBBC phase I study of gemcitabine and continuous infusion 5-fluorouracil in patients with metastatic breast cancer resistant to anthracyclines or pre-treated with both anthracyclines and taxanes. The aim of this study was to determine the maximum tolerated dose (MTD), dose-limiting toxicities (DLT), and potential activity of combined gemcitabine and continuous infusion 5-fluorouracil (5-FU) in metastatic breast cancer (MBC) patients that a...

Hanthamrongwit, M.; Reid, W.H.; Grant, M.H., 1996: Chondroitin-6-sulphate incorporated into collagen gels for the growth of human keratinocytes: The effect of cross-linking agents and diamines. This study demonstrates the effect of the glycosaminoglycans, hyaluronic acid and chondroitin-6-sulphate (Ch6SO-4), diamines and a carbodiimide cross-linking agent on the growth of human epidermal cells on collagen gels. Ch6SO-4 incorporated into...