- POLYMORPHIC COMPOUNDS AND USES THEREOF
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The present invention provides compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.
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- COMPOUNDS AND METHODS FOR TREATING ADDICTION AND RELATED DISORDERS
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The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example an addiction or compulsive disorder.
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- Compounds and methods for treating neurological and cardiovascular conditions
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The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.
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- NON-RIBOSE CONTAINING INHIBITORS OF HISTONE METHYLTRANSFERASE DOT1L FOR CANCER TREATMENT
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A compound of Formula I, a pharmaceutically acceptable salt thereof, a prodrug thereof, or combinations thereof: wherein R1 is H, methyl, or benzyl: R2 is 2-cyanoethyl, 2-methoxycarbonylethyl, or 2-iodoethyl; X is N or S; wherein if
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- Synthesis, activity and metabolic stability of non-ribose containing inhibitors of histone methyltransferase DOT1L
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Histone methyltransferase DOT1L is a drug target for MLL leukemia. We report an efficient synthesis of a cyclopentane-containing compound that potently and selectively inhibits DOT1L (Ki = 1.1 nM) as well as H3K79 methylation (IC50 ~
- Deng, Lisheng,Zhang, Li,Yao, Yuan,Wang, Cong,Redell, Michele S.,Dong, Shuo,Song, Yongcheng
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p. 822 - 826
(2013/08/26)
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- Total syntheses of a conformationally locked North-type methanocarba puromycin analogue and a dinucleotide derivative
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An original synthetic approach for the first synthesis of an enantiopure methanocarba puromycin (3'-α-aminoacylamino-3'-deoxyadenosine) analogue and its cytidine dinucleotide derivative is described. Each compound is conformationally locked in a North-typ
- Michel, Benoit Y.,Strazewski, Peter
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supporting information; experimental part
p. 6244 - 6257
(2010/03/26)
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- Synthesis of (-)-neplanocin A with the highest overall yield via an efficient Mitsunobu coupling
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Neplanocin A was synthesized in very high isolated yield and purity, in 10 steps from d-ribose via an efficient Mitsunobu coupling using N6-bis-Boc-protected adenine. In fact, this synthesis is a short pathway to enantiopure neplanocin A giving
- Michel, Beno?t Y.,Strazewski, Peter
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p. 9836 - 9841
(2008/02/11)
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- Stereoselective synthesis of 3-hydroxymethyl-D-cyclopentenone, the versatile intermediate for the synthesis of carbocyclic nucleosides
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The preparative and stereoselective synthesis (45-50% overall yields, >50 g scale) of the key carbasugars 7a-d was achieved from D-ribose via stereoselective Grignard reaction and oxidative rearrangement as key reactions. Copyright Taylor & Francis, Inc.
- Choi, Won Jun,Moon, Hyung Ryong,Kim, Hea Ok,Ko, Young Mi,Kim, Hye Jin,Lee, Jeong A.,Lee, Kang Man,Yun, Mi Kyung,Shin, Dae Hong,Chun, Moon Woo,Sheen, Yhun Y.,Kim, Kilhyoun,Jeong, Lak Shin
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p. 611 - 613
(2008/02/04)
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- Preparative and Stereoselective Synthesis of the Versatile Intermediate for Carbocyclic Nucleosides: Effects of the Bulky Protecting Groups to Enforce Facial Selectivity
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The preparative and stereoselective synthesis (45-50% overall yields) of the target compound 17 has been accomplished from D-ribose. The bulky protecting groups such as TBDPS and Trityl enforced the facial selectivity during Grignard reaction to give the
- Choi, Won Jun,Moon, Hyung Ryong,Kim, Hea Ok,Yoo, Byul Nae,Lee, Jeong A.,Shin, Dae Hong,Jeong, Lak Shin
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p. 2634 - 2636
(2007/10/03)
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