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Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.
TLDR
A novel homology model of the kinase domain of Janus kinase (JAK) 3 was used for the structure-based design of dimethoxyquinazoline compounds with potent and specific inhibitory activity against JAK3, and derivatives of this compound that contain an OH group at the 4' position of the phenyl ring may provide the new treatment strategies for the design of childhood treatment strategies.
Rational Design and Synthesis of a Novel Anti-leukemic Agent Targeting Bruton′s Tyrosine Kinase (BTK), LFM-A13 [α-Cyano-β-Hydroxy-β-Methyl-N-(2,5-Dibromophenyl)Propenamide]*
TLDR
Treatment of BTK+ B-lineage leukemic cells with LFM-A13 enhanced their sensitivity to ceramide- or vincristine-induced apoptosis and is the first BTK-specific tyrosine kinase inhibitor and the first anti-leukemic agent targeting BTK.
Rational Design and Synthesis of a Novel Anti-leukemic Agent Targeting
In a systematic effort to design potent inhibitors of the anti-apoptotic tyrosine kinase BTK (Bruton*s tyrosine kinase) as anti-leukemic agents with apoptosis-promoting and chemosensitizing
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
TLDR
HI-236 was highly effective against the multidrug-resistant HIV-1 strain RT-MDR with multiple mutations involving the RT residues 74V, 41L, 106A, and 215Y and twice as effective as the recently reported lead compound N-[2-fluorophenethyl]-N'-[2-(5-bromopyridyl)]-thiourea.
Structure-Based Design of Novel Dihydroalkoxybenzyloxopyrimidine Derivatives as Potent Nonnucleoside Inhibitors of the Human Immunodeficiency Virus Reverse Transcriptase
ABSTRACT Two highly potent dihydroalkoxybenzyloxopyrimidine (DABO) derivatives targeting the nonnucleoside inhibitor (NNI) binding site of human immunodeficiency virus (HIV) reverse transcriptase
Structure-based drug design of non-nucleoside inhibitors for wild-type and drug-resistant HIV reverse transcriptase.
TLDR
It is revealed that for an NNI of HIV RT to be active againstRT mutants such as the especially problematic Y181C RT mutant, the following features are required: the inhibitor should be highly potent against wild-type RT and therefore capable of tolerating a considerable activity loss against RT mutants, and the inhibitors should contain functional groups that provide favorable chemical interactions with Wing 2 residues of wild- type as well as mutant RT.
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.
In this Letter we describe the optimization of an aminopurine lead (1) with modest potency and poor overall kinase selectivity which led to the identification of a series of potent, selective JNK
SPIKET and COBRA compounds as novel tubulin modulators with potent anticancer activity.
  • F. Uckun, C. Mao, +5 authors R. Narla
  • Medicine, Chemistry
    Current opinion in investigational drugs
  • 1 October 2000
TLDR
COBRA and SPIKET compounds represent two new classes of tubulin targeting agents that show promise as anticancer drugs.
Alpha-cyano-beta-hydroxy-beta-methyl-N-[4-(trifluoromethoxy)phenyl] propenamide: an inhibitor of the epidermal growth factor receptor tyrosine kinase with potent cytotoxic activity against breast
  • S. Ghosh, Y. Zheng, +6 authors F. Uckun
  • Biology, Medicine
    Clinical cancer research : an official journal of…
  • 1 November 1998
TLDR
A homology model is constructed to represent the structure of EGF-R and it is proposed that this model can be used to design potent inhibitors of E GF-R, which may provide the basis for the development of a new class of potent and clinically useful anti-breast cancer agents.
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