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Items: 13

1.

Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.

Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M, Sameshima T, Araki S, Endo S, Kawamoto T, Morin GB, Aparicio SA, Nakanishi A, Maezaki H, Imaeda Y.

J Med Chem. 2018 Sep 13;61(17):7710-7728. doi: 10.1021/acs.jmedchem.8b00683. Epub 2018 Aug 20.

PMID:
30067358
2.

Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability.

Iwai K, Yaguchi M, Nishimura K, Yamamoto Y, Tamura T, Nakata D, Dairiki R, Kawakita Y, Mizojiri R, Ito Y, Asano M, Maezaki H, Nakayama Y, Kaishima M, Hayashi K, Teratani M, Miyakawa S, Iwatani M, Miyamoto M, Klein MG, Lane W, Snell G, Tjhen R, He X, Pulukuri S, Nomura T.

EMBO Mol Med. 2018 Jun;10(6). pii: e8289. doi: 10.15252/emmm.201708289.

3.

Discovery of Novel Selective Acetyl-CoA Carboxylase (ACC) 1 Inhibitors.

Mizojiri R, Asano M, Tomita D, Banno H, Nii N, Sasaki M, Sumi H, Satoh Y, Yamamoto Y, Moriya T, Satomi Y, Maezaki H.

J Med Chem. 2018 Feb 8;61(3):1098-1117. doi: 10.1021/acs.jmedchem.7b01547. Epub 2018 Jan 5.

PMID:
29232514
4.

Discovery of spiro[indole-3,2'-pyrrolidin]-2(1H)-one based inhibitors targeting Brr2, a core component of the U5 snRNP.

Ito M, Iwatani M, Yamamoto T, Tanaka T, Kawamoto T, Morishita D, Nakanishi A, Maezaki H.

Bioorg Med Chem. 2017 Sep 1;25(17):4753-4767. doi: 10.1016/j.bmc.2017.07.017. Epub 2017 Jul 13.

PMID:
28751196
5.

Discovery of Allosteric Inhibitors Targeting the Spliceosomal RNA Helicase Brr2.

Iwatani-Yoshihara M, Ito M, Klein MG, Yamamoto T, Yonemori K, Tanaka T, Miwa M, Morishita D, Endo S, Tjhen R, Qin L, Nakanishi A, Maezaki H, Kawamoto T.

J Med Chem. 2017 Jul 13;60(13):5759-5771. doi: 10.1021/acs.jmedchem.7b00461. Epub 2017 Jun 20.

PMID:
28586220
6.

Design of potent dipeptidyl peptidase IV (DPP-4) inhibitors by employing a strategy to form a salt bridge with Lys554.

Maezaki H, Tawada M, Yamashita T, Banno Y, Miyamoto Y, Yamamoto Y, Ikedo K, Kosaka T, Tsubotani S, Tani A, Asakawa T, Suzuki N, Oi S.

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3565-3571. doi: 10.1016/j.bmcl.2017.05.048. Epub 2017 May 17.

PMID:
28579121
7.

Discovery of Novel and Potent Stearoyl Coenzyme A Desaturase 1 (SCD1) Inhibitors as Anticancer Agents.

Imamura K, Tomita N, Kawakita Y, Ito Y, Ono K, Nii N, Miyazaki T, Yonemori K, Tawada M, Sumi H, Satoh Y, Yamamoto Y, Miyahisa I, Sasaki M, Satomi Y, Hirayama M, Nishigaki R, Maezaki H.

Bioorg Med Chem. 2017 Jul 15;25(14):3768-3779. doi: 10.1016/j.bmc.2017.05.016. Epub 2017 May 11.

PMID:
28571972
8.

In vitro and in vivo antitumor activities of T-3764518, a novel and orally available small molecule stearoyl-CoA desaturase 1 inhibitor.

Nishizawa S, Sumi H, Satoh Y, Yamamoto Y, Kitazawa S, Honda K, Araki H, Kakoi K, Imamura K, Sasaki M, Miyahisa I, Satomi Y, Nishigaki R, Hirayama M, Aoyama K, Maezaki H, Hara T.

Eur J Pharmacol. 2017 Jul 15;807:21-31. doi: 10.1016/j.ejphar.2017.03.064. Epub 2017 Apr 22.

PMID:
28442322
9.

Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.

Shirai J, Sugiyama H, Morimoto S, Maezaki H, Yamamoto Y, Okanishi S, Kamo I, Matsumoto S, Ishigami K, Inatomi N, Imanishi A, Kawamoto M, Tarui N, Hashimoto T, Ikeura Y.

Bioorg Med Chem. 2012 Jan 15;20(2):962-77. doi: 10.1016/j.bmc.2011.11.048. Epub 2011 Dec 1.

PMID:
22189275
10.

Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554.

Banno Y, Miyamoto Y, Sasaki M, Oi S, Asakawa T, Kataoka O, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Tsubotani S, Tani A, Funami M, Tawada M, Yamamoto Y, Aertgeerts K, Yano J, Maezaki H.

Bioorg Med Chem. 2011 Aug 15;19(16):4953-70. doi: 10.1016/j.bmc.2011.06.059. Epub 2011 Jun 28.

PMID:
21764322
11.

Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554.

Maezaki H, Banno Y, Miyamoto Y, Moritoh Y, Asakawa T, Kataoka O, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Sasaki M, Tsubotani S, Tani A, Funami M, Yamamoto Y, Tawada M, Aertgeerts K, Yano J, Oi S.

Bioorg Med Chem. 2011 Aug 1;19(15):4482-98. doi: 10.1016/j.bmc.2011.06.032. Epub 2011 Jul 7. Erratum in: Bioorg Med Chem. 2011 Sep 15;19(18):5742. Moritou, Yuusuke [corrected to Moritoh, Yusuke].

PMID:
21741847
12.

Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor.

Miyamoto Y, Banno Y, Yamashita T, Fujimoto T, Oi S, Moritoh Y, Asakawa T, Kataoka O, Yashiro H, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Tsubotani S, Tani A, Sasaki M, Funami M, Amano M, Yamamoto Y, Aertgeerts K, Yano J, Maezaki H.

J Med Chem. 2011 Feb 10;54(3):831-50. doi: 10.1021/jm101236h. Epub 2011 Jan 10.

PMID:
21218817
13.

Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125.

Miyamoto Y, Banno Y, Yamashita T, Fujimoto T, Oi S, Moritoh Y, Asakawa T, Kataoka O, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Tsubotani S, Tani A, Funami M, Amano M, Yamamoto Y, Aertgeerts K, Yano J, Maezaki H.

Bioorg Med Chem. 2011 Jan 1;19(1):172-85. doi: 10.1016/j.bmc.2010.11.038. Epub 2010 Nov 25.

PMID:
21163664

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