408355-02-2Relevant articles and documents
Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor γ/δ agonists We dedicate this article to Professor Young-Ger Suh on the occasion of his retirement.
Gim, Hyo Jin,Li, Hua,Jeong, Ji Hye,Lee, Su Jeong,Sung, Mi-Kyung,Song, Mi-Young,Park, Byung-Hyun,Oh, Soo Jin,Ryu, Jae-Ha,Jeon, Raok
, p. 3322 - 3336 (2015)
Abstract A series of alkoxy-3-indolylacetic acid analogs has been discovered as peroxisome proliferator-activated receptor (PPAR) agonists. Structure-activity relationship study indicated that PPARα/γ/δ activities were dependent on the nature of the hydrophobic group, the attachment position of the alkoxy linker to the indole ring, and N-alkylation of indole nitrogen. Some compounds presented significant PPARγ/δ activity and molecular modeling suggested their putative binding modes in the ligand binding domain of PPARγ. Of these, compound 51 was selected for in vivo study via an evaluation of microsomal stability in mouse and human liver. Compound 51 lowered the levels of fasting blood glucose, insulin, and HbA1c without gain in body weight in db/db mice. When compound 51 was treated, hepatic triglycerides level and the size of adipocytes in white adipose tissue of db/db mice were also reduced as opposed to treatment with rosiglitazone. Taken together, compound 51 shows high potential warranting further studies in models for diabetes and related metabolic disorders and may be in use as a chemical tool for the understanding of PPAR biology.
Novel, potent and selective cyclin D1/CDK4 inhibitors: Indolo[6,7-a]pyrrolo[3,4-c]carbazoles
Engler, Thomas A.,Furness, Kelly,Malhotra, Sushant,Sanchez-Martinez, Concha,Shih, Chuan,Xie, Walter,Zhu, Guoxin,Zhou, Xun,Conner, Scott,Faul, Margaret M.,Sullivan, Kevin A.,Kolis, Stanley P.,Brooks, Harold B.,Patel, Bharvin,Schultz, Richard M.,DeHahn, Tammy B.,Kirmani, Kashif,Spencer, Charles D.,Watkins, Scott A.,Considine, Eileen L.,Dempsey, Jack A.,Ogg, Catherine A.,Stamm, Nancy B.,Anderson, Bryan D.,Campbell, Robert M.,Vasudevan, Vasu,Lytle, Michelle L.
, p. 2261 - 2267 (2007/10/03)
The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.
