106157-94-2

One compound sometimes shows two biological functions, becoming important aspect of recent drug discovery. This study began with an attempt to confirm the previously reported molecular mechanism of the anti-human immunodeficiency virus (HIV) heterocyclic compound BMMP [2-(benzothiazol-2-ylmethylthio)-4-methylpyrimidine], i.e., induction of abnormal uncoating of the viral core at the post-entry step. Our mechanistic study gave results consistent with this mechanism. We further attempted to find out the molecular target of BMMP by a pulldown approach using previously synthesized biotinylated BMMP (Biotin-BMMP) and successfully identified heterogenous nuclear ribonucleoprotein M (hnRNP M) as a BMMP-binding protein. This protein was found not to be accountable for the anti-HIV activity of BMMP. As hnRNP M has been reported to promote cancer metastasis, we tested this mechanism and found that BMMP suppressed migration of the human lung carcinoma cell line A549 stimulated with transforming growth factor-β (TGF-β). Mechanistic study showed that BMMP suppressed the expression of CD44 mRNA via the regulation of hnRNP M. Furthermore, six new derivatives of BMMP were synthesized, and the patterns of their activities against HIV-1 and cell migration were not uniform, suggesting that the anti-HIV mechanism and the anti-cell migration mechanism of BMMP are independent. Taken together, the anti-cell migration activity of the anti-HIV heterocyclic compound BMMP was newly discovered by identification of its binding protein hnRNP M using a chemical biology approach.

There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof,wherein the ring containing Q1to Q5, and the groups R1, R2 and R3, have meanings as provided in the description.

The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5 and R6 are as defined in the specification or a pharmaceutically acceptable salt or solvate thereof, compositions thereof,

Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.

Compounds represented by formula (I) wherein A, R1, R2, R3, and R4 are as defined in the specification, compositions thereof, and methods of use thereof.

The present invention is directed to the substantially pure compound of formula (A), or pharmaceutically acceptable salt, or solvate of said compound; to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formul

Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be

The present invention is directed to the substantially pure compound of formula (A), or pharmaceutically acceptable salt, or solvate of said compound; to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formul

The present invention relates to a compound of the formula [I] : ???wherein G1 is an alkyl which,may be substituted by a halogen atom or an alkoxy, or a group of the formula: ??????wherein ring B is benzene ring which may be substituted, etc.,

The invention relates to compounds of formula (I). Said compounds are suitable for producing medicaments for the prophylaxis and treatment of diseases, the progression of which involves increased activity of IκB kinase.

The synthesis of the four possible 2-amino- and 2-guanidino-4-(2-amino- and 2-guanidinothiazolyl)pyrimidines is described and pKa values are calculated.Guanidinopyrimidines are more basic than guanidinothiazoles.However, the reverse is true of the corresponding amino heterocycles; the amino thiazole is more basic than the amino pyrimidine.