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Page 1
Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.
He S, Lai Z, Ye Z, Dobbelaar PH, Shah SK, Truong Q, Du W, Guo L, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Reibarkh M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang B, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: mitelman s. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53. doi: 10.1021/ml500028c. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050159 Free PMC article.
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: mitelman s. ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900499 Free PMC article.
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Shah SK, He S, Guo L, Truong Q, Qi H, Du W, Lai Z, Liu J, Jian T, Hong Q, Dobbelaar P, Ye Z, Sherer E, Feng Z, Yu Y, Wong F, Samuel K, Madiera M, Karanam BV, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Feng Y, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Pachanski M, Fernandez G, Nelson D, Bunting P, Morissette P, Volksdorf S, Kerr J, Zhang BB, Howard AD, Zhou YP, Pasternak A, Nargund RP, Hagmann WK. Shah SK, et al. Among authors: mitelman s. ACS Med Chem Lett. 2015 Mar 18;6(5):513-7. doi: 10.1021/ml500514w. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005524 Free PMC article.
SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists.
He S, Dobbelaar PH, Guo L, Ye Z, Liu J, Jian T, Truong Q, Shah SK, Du W, Qi H, Bakshi RK, Hong Q, Dellureficio JD, Sherer E, Pasternak A, Feng Z, Reibarkh M, Lin M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: mitelman s. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-1535. doi: 10.1016/j.bmcl.2016.02.022. Epub 2016 Feb 10. Bioorg Med Chem Lett. 2016. PMID: 26898814
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D. Guo L, et al. Among authors: mitelman s. ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994747 Free PMC article.
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines.
Ouyang X, Piatnitski EL, Pattaropong V, Chen X, He HY, Kiselyov AS, Velankar A, Kawakami J, Labelle M, Smith L 2nd, Lohman J, Lee SP, Malikzay A, Fleming J, Gerlak J, Wang Y, Rosler RL, Zhou K, Mitelman S, Camara M, Surguladze D, Doody JF, Tuma MC. Ouyang X, et al. Among authors: mitelman s. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1191-6. doi: 10.1016/j.bmcl.2005.11.094. Epub 2006 Jan 11. Bioorg Med Chem Lett. 2006. PMID: 16377187
Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2.
Duncton MA, Piatnitski Chekler EL, Katoch-Rouse R, Sherman D, Wong WC, Smith LM 2nd, Kawakami JK, Kiselyov AS, Milligan DL, Balagtas C, Hadari YR, Wang Y, Patel SN, Rolster RL, Tonra JR, Surguladze D, Mitelman S, Kussie P, Bohlen P, Doody JF. Duncton MA, et al. Among authors: mitelman s. Bioorg Med Chem. 2009 Jan 15;17(2):731-40. doi: 10.1016/j.bmc.2008.11.049. Epub 2008 Nov 24. Bioorg Med Chem. 2009. PMID: 19101155
Antitumor Activity of IMC-038525, a Novel Oral Tubulin Polymerization Inhibitor.
Tuma MC, Malikzay A, Ouyang X, Surguladze D, Fleming J, Mitelman S, Camara M, Finnerty B, Doody J, Chekler EL, Kussie P, Tonra JR. Tuma MC, et al. Among authors: mitelman s. Transl Oncol. 2010 Oct 1;3(5):318-25. doi: 10.1593/tlo.10160. Transl Oncol. 2010. PMID: 20885894 Free PMC article.
57 results