Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors

被引：22

作者：

Singh, Baljinder ^{[1
]}

Bernatchez, Jean A. ^{[2
]}

McCall, Laura-Isobel ^{[2
]}

Calvet, Claudia M. ^{[2
]}

Ackermann, Jasmin ^{[2
]}

Souza, Julia M. ^{[2
]}

Thomas, Diane ^{[2
]}

Silva, Everton M. ^{[2
]}

Bachovchin, Kelly A. ^{[1
]}

Klug, Dana M. ^{[1
]}

Jalani, Hitesh B. ^{[1
]}

Bag, Seema ^{[1
]}

Buskes, Melissa J. ^{[1
]}

Leed, Susan E. ^{[3
]}

Roncal, Norma E. ^{[3
]}

Penn, Erica C. ^{[3
]}

Erath, Jessey ^{[4
]}

Rodriguez, Ana ^{[4
]}

Sciotti, Richard J. ^{[3
]}

Campbell, Robert F. ^{[3
]}

McKerrow, James ^{[2
]}

Siqueira-Neto, Jair L. ^{[2
]}

Ferrins, Lori ^{[1
]}

Pollastri, Michael P. ^{[1
]}

机构：

[1] Northeastern Univ, Dept Chem & Chem Biol, Boston, MA 02115 USA

[2] Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, La Jolla, CA 92093 USA

[3] Walter Reed Army Inst Res, Expt Therapeut, Silver Spring, MD 20910 USA

[4] NYU, Sch Med, Dept Microbiol, New York, NY 10010 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2020年 / 11卷 / 03期

基金：

美国国家卫生研究院;

关键词：

Kinetoplastids; leishmaniasis; Chagas disease; malaria; protozoan parasite inhibitors; parasite-hopping; NEGLECTED TROPICAL DISEASES; DRUG DISCOVERY; LEAD;

D O I：

10.1021/acsmedchemlett.9b00453

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.

引用

页码：249 / 257

页数：9

共 15 条

[1] Heart Failure in South America
Alcides Bocchi, Edimar
[J]. CURRENT CARDIOLOGY REVIEWS, 2013, 9 (02) : 147 - 156
[2] Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development
Bachoychin, Kelly A.
Sharma, Amrita
Bag, Seema
Klug, Dana M.
Schneider, Katherine M.
Singh, Baljinder
Jalani, Hitesh B.
Buskes, Melissa J.
Mehta, Naimee
Tanghe, Scott
Momper, Jeremiah D.
Sciotti, Richard J.
Rodriguez, Ana
Mensa-Wilmot, Kojo
Pollastri, Michael P.
Ferrins, Lori
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2019, 62 (02) : 665 - 687
[3] Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites
Devine, William
Thomas, Sarah M.
Erath, Jessey
Bachovchin, Kelly A.
Lee, Patricia J.
Leed, Susan E.
Rodriguez, Ana
Sciotti, Richard J.
Mensa-Wilmot, Kojo
Pollastri, Michael P.
[J]. ACS MEDICINAL CHEMISTRY LETTERS, 2017, 8 (03): : 350 - 354
[4] Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery
Devine, William
Woodring, Jennifer L.
Swaminathan, Uma
Amata, Emanuele
Patel, Gautam
Erath, Jessey
Roncal, Norma E.
Lee, Patricia J.
Leed, Susan E.
Rodriguez, Ana
Mensa-Wilmot, Kojo
Sciotti, Richard J.
Pollastri, Michael P.
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (14) : 5522 - 5537
[5] Anilinoquinoline based inhibitors of trypanosomatid proliferation
Ferrins, Lori
Sharma, Amrita
Thomas, Sarah M.
Mehta, Naimee
Erath, Jessey
Tanghe, Scott
Leed, Susan E.
Rodriguez, Ana
Mensa-Wilmot, Kojo
Sciotti, Richard J.
Gillingwater, Kirsten
Pollastri, Michael P.
[J]. PLOS NEGLECTED TROPICAL DISEASES, 2018, 12 (11):
[6] Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need
Field, Mark C.
Horn, David
Fairlamb, Alan H.
Ferguson, Michael A. J.
Gray, David W.
Read, Kevin D.
De Rycker, Manu
Torrie, Leah S.
Wyatt, Paul G.
Wyllie, Susan
Gilbert, Ian H.
[J]. NATURE REVIEWS MICROBIOLOGY, 2017, 15 (04) : 217 - 231
[7] Gyapong JO, 2016, NEGLECT TROP DIS, P1, DOI 10.1007/978-3-319-25471-5_1
[8] Hit and lead criteria in drug discovery for infectious diseases of the developing world
Katsuno, Kei
Burrows, Jeremy N.
Duncan, Ken
van Huijsduijnen, Rob Hooft
Kaneko, Takushi
Kita, Kiyoshi
Mowbray, Charles E.
Schmatz, Dennis
Warner, Peter
Slingsby, B. T.
[J]. NATURE REVIEWS DRUG DISCOVERY, 2015, 14 (11) : 751 - 758
[9] Repurposing strategies for tropical disease drug discovery
Klug, Dana M.
Gelb, Michael H.
Pollastri, Michael P.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (11) : 2569 - 2576
[10] Emerging and Reemerging Neglected Tropical Diseases: a Review of Key Characteristics, Risk Factors, and the Policy and Innovation Environment
Mackey, Tim K.
Liang, Bryan A.
Cuomo, Raphael
Hafen, Ryan
Brouwer, Kimberly C.
Lee, Daniel E.
[J]. CLINICAL MICROBIOLOGY REVIEWS, 2014, 27 (04) : 949 - 979

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