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Items: 1 to 20 of 118

1.

Formation of 5α-dihydrotestosterone from 5α-androstane-3α,17β-diol in prostate cancer LAPC-4 cells - Identifying inhibitors of non-classical pathways producing the most potent androgen.

Boutin S, Roy J, Maltais R, Poirier D.

Bioorg Med Chem Lett. 2019 Nov 9:126783. doi: 10.1016/j.bmcl.2019.126783. [Epub ahead of print]

PMID:
31753699
2.

A- and D-Ring Structural Modifications of an Androsterone Derivative Inhibiting 17β-Hydroxysteroid Dehydrogenase Type 3: Chemical Synthesis and Structure-Activity Relationships.

Cortés-Benítez F, Roy J, Perreault M, Maltais R, Poirier D.

J Med Chem. 2019 Aug 8;62(15):7070-7088. doi: 10.1021/acs.jmedchem.9b00624. Epub 2019 Jul 19.

PMID:
31268309
3.

Antisulfatase, Osteogenic, and Anticancer Activities of Steroid Sulfatase Inhibitor EO-33 in Mice.

Poirier D, Roy J, Maltais R, Ayan D.

J Med Chem. 2019 Jun 13;62(11):5512-5521. doi: 10.1021/acs.jmedchem.9b00382. Epub 2019 May 22.

PMID:
31062594
4.

Isolation and functional characterization of a novel endogenous inverse agonist of estrogen related receptors (ERRs) from human pregnancy urine.

Ghanbari F, Hebert-Losier A, Barry J, Poirier D, Giguere V, Mader S, Philip A.

J Steroid Biochem Mol Biol. 2019 Jul;191:105352. doi: 10.1016/j.jsbmb.2019.04.001. Epub 2019 Apr 5.

PMID:
30954508
5.

Total Synthesis of the Antidiabetic (Type 2) Lipid Mediator Protectin DX/PDX.

Sancéau JY, Maltais R, Poirier D, Marette A.

J Org Chem. 2019 Jan 18;84(2):495-505. doi: 10.1021/acs.joc.8b01973. Epub 2018 Dec 26.

PMID:
30586310
6.

Identification of steroidal derivatives inhibiting the transformations of allopregnanolone and estradiol by 17β-hydroxysteroid dehydrogenase type 10.

Boutin S, Roy J, Maltais R, Alata W, Calon F, Poirier D.

Bioorg Med Chem Lett. 2018 Dec 1;28(22):3554-3559. doi: 10.1016/j.bmcl.2018.09.031. Epub 2018 Sep 26.

PMID:
30297283
7.

Chemical synthesis of C3-oxiranyl/oxiranylmethyl-estrane derivatives targeted by molecular modeling and tested as potential inhibitors of 17β-hydroxysteroid dehydrogenase type 1.

Lespérance M, Barbeau X, Roy J, Maltais R, Lagüe P, Poirier D.

Steroids. 2018 Dec;140:104-113. doi: 10.1016/j.steroids.2018.09.009. Epub 2018 Sep 28.

PMID:
30273695
8.

Targeting Cytochrome P450 (CYP) 1B1 Enzyme with Four Series of A-Ring Substituted Estrane Derivatives: Design, Synthesis, Inhibitory Activity, and Selectivity.

Dutour R, Roy J, Cortés-Benítez F, Maltais R, Poirier D.

J Med Chem. 2018 Oct 25;61(20):9229-9245. doi: 10.1021/acs.jmedchem.8b00907. Epub 2018 Oct 3.

PMID:
30216063
9.

Combined Biophysical Chemistry Reveals a New Covalent Inhibitor with a Low-Reactivity Alkyl Halide.

Li T, Maltais R, Poirier D, Lin SX.

J Phys Chem Lett. 2018 Sep 20;9(18):5275-5280. doi: 10.1021/acs.jpclett.8b02225. Epub 2018 Aug 31.

PMID:
30148957
10.

Induction of endoplasmic reticulum stress by aminosteroid derivative RM-581 leads to tumor regression in PANC-1 xenograft model.

Perreault M, Maltais R, Roy J, Picard S, Popa I, Bertrand N, Poirier D.

Invest New Drugs. 2019 Jun;37(3):431-440. doi: 10.1007/s10637-018-0643-4. Epub 2018 Jul 30.

PMID:
30062573
11.

Steroid sulfatase inhibition success and limitation in breast cancer clinical assays: An underlying mechanism.

Sang X, Han H, Poirier D, Lin SX.

J Steroid Biochem Mol Biol. 2018 Oct;183:80-93. doi: 10.1016/j.jsbmb.2018.05.009. Epub 2018 May 24.

PMID:
29803725
12.

Parallel Solid-Phase Synthesis using a New Diethylsilylacetylenic Linker and Leading to Mestranol Derivatives with Potent Antiproliferative Activities on Multiple Cancer Cell Lines.

Dutour R, Maltais R, Perreault M, Roy J, Poirier D.

Anticancer Agents Med Chem. 2018;18(10):1469-1481. doi: 10.2174/1871520618666180307130158.

PMID:
29521249
13.

Implication of STARD5 and cholesterol homeostasis disturbance in the endoplasmic reticulum stress-related response induced by pro-apoptotic aminosteroid RM-133.

Perreault M, Maltais R, Kenmogne LC, Létourneau D, LeHoux JG, Gobeil S, Poirier D.

Pharmacol Res. 2018 Feb;128:52-60. doi: 10.1016/j.phrs.2017.12.024. Epub 2017 Dec 26.

PMID:
29287690
14.

Pharmacokinetic profile of PBRM in rodents, a first selective covalent inhibitor of 17β-HSD1 for breast cancer and endometriosis treatments.

Maltais R, Trottier A, Roy J, Ayan D, Bertrand N, Poirier D.

J Steroid Biochem Mol Biol. 2018 Apr;178:167-176. doi: 10.1016/j.jsbmb.2017.12.007. Epub 2017 Dec 14.

PMID:
29248731
15.

Structure-Based Design and Synthesis of New Estrane-Pyridine Derivatives as Cytochrome P450 (CYP) 1B1 Inhibitors.

Dutour R, Cortés-Benítez F, Roy J, Poirier D.

ACS Med Chem Lett. 2017 Oct 11;8(11):1159-1164. doi: 10.1021/acsmedchemlett.7b00265. eCollection 2017 Nov 9.

16.

Insight into the mode of action and selectivity of PBRM, a covalent steroidal inhibitor of 17β-hydroxysteroid dehydrogenase type 1.

Trottier A, Maltais R, Ayan D, Barbeau X, Roy J, Perreault M, Poulin R, Lagüe P, Poirier D.

Biochem Pharmacol. 2017 Nov 15;144:149-161. doi: 10.1016/j.bcp.2017.08.004. Epub 2017 Aug 9.

PMID:
28800957
17.

Inhibitors of cytochrome P450 (CYP) 1B1.

Dutour R, Poirier D.

Eur J Med Chem. 2017 Jul 28;135:296-306. doi: 10.1016/j.ejmech.2017.04.042. Epub 2017 Apr 18. Review.

PMID:
28458135
18.

Impact of androstane A- and D-ring inversion on 17β-hydroxysteroid dehydrogenase type 3 inhibitory activity, androgenic effect and metabolic stability.

Cortés-Benítez F, Roy J, Maltais R, Poirier D.

Bioorg Med Chem. 2017 Apr 1;25(7):2065-2073. doi: 10.1016/j.bmc.2017.02.008. Epub 2017 Feb 9.

PMID:
28254377
19.

Investigation of the In Vitro and In Vivo efficiency of RM-532-105, a 17β-hydroxysteroid dehydrogenase type 3 inhibitor, in LAPC-4 prostate cancer cell and tumor models.

Kenmogne LC, Roy J, Maltais R, Rouleau M, Neveu B, Pouliot F, Poirier D.

PLoS One. 2017 Feb 9;12(2):e0171871. doi: 10.1371/journal.pone.0171871. eCollection 2017.

20.

Design of a Mestranol 2-N-Piperazino-Substituted Derivative Showing Potent and Selective in vitro and in vivo Activities in MCF-7 Breast Cancer Models.

Perreault M, Maltais R, Roy J, Dutour R, Poirier D.

ChemMedChem. 2017 Jan 20;12(2):177-182. doi: 10.1002/cmdc.201600482. Epub 2017 Jan 6.

PMID:
28060448

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