Heterocyclic scaffolds: centrality in anticancer drug development
I Ali, M Nadeem Lone, Z A. Al-Othman… - Current drug …, 2015 - benthamdirect.com
Cancer has been cursed for human beings for long time. Millions people lost their lives due
to cancer. Despite of the several anticancer drugs available, cancer cannot be cured; …
to cancer. Despite of the several anticancer drugs available, cancer cannot be cured; …
Thiazolidine-2, 4-diones as multi-targeted scaffold in medicinal chemistry: Potential anticancer agents
A variety of substituents on the thiazolidine-2, 4-dione (TZD) nucleus have provided a wide
spectrum of biological activities by the using of different mechanism on various target sites …
spectrum of biological activities by the using of different mechanism on various target sites …
AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia
EK Keeton, K McEachern, KS Dillman… - Blood, The Journal …, 2014 - ashpublications.org
Upregulation of Pim kinases is observed in several types of leukemias and lymphomas. Pim-
1,-2, and-3 promote cell proliferation and survival downstream of cytokine and growth factor …
1,-2, and-3 promote cell proliferation and survival downstream of cytokine and growth factor …
Pim2 is required for maintaining multiple myeloma cell growth through modulating TSC2 phosphorylation
J Lu, T Zavorotinskaya, Y Dai, XH Niu… - Blood, The Journal …, 2013 - ashpublications.org
Multiple myeloma (MM) is the second most common hematologic malignancy. Despite
recent treatment advances, it remains incurable. Here, we report that Pim2 kinase …
recent treatment advances, it remains incurable. Here, we report that Pim2 kinase …
Pim kinases in cancer: diagnostic, prognostic and treatment opportunities
C Blanco-Aparicio, A Carnero - Biochemical pharmacology, 2013 - Elsevier
PIM proteins belong to a family of ser/thr kinases composed of 3 members, PIM1, PIM2 and
PIM3, with greatly overlapping functions. PIM kinases are mainly responsible for cell cycle …
PIM3, with greatly overlapping functions. PIM kinases are mainly responsible for cell cycle …
Phase I studies of AZD1208, a proviral integration Moloney virus kinase inhibitor in solid and haematological cancers
J Cortes, K Tamura, DJ DeAngelo, J De Bono… - British journal of …, 2018 - nature.com
Abstract Background Proviral integration Moloney virus (PIM) kinases (PIM1, 2 and 3) are
overexpressed in several tumour types and contribute to oncogenesis. AZD1208 is a potent …
overexpressed in several tumour types and contribute to oncogenesis. AZD1208 is a potent …
Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers
PD Garcia, JL Langowski, Y Wang, M Chen… - Clinical cancer …, 2014 - AACR
Purpose: PIM kinases have been shown to act as oncogenes in mice, with each family
member being able to drive progression of hematologic cancers. Consistent with this, we …
member being able to drive progression of hematologic cancers. Consistent with this, we …
STAT5 is essential for IL-7–mediated viability, growth, and proliferation of T-cell acute lymphoblastic leukemia cells
T-cell acute lymphoblastic leukemia (T-ALL) constitutes an aggressive subset of ALL, the
most frequent childhood malignancy. Whereas interleukin-7 (IL-7) is essential for normal T …
most frequent childhood malignancy. Whereas interleukin-7 (IL-7) is essential for normal T …
PIM kinase inhibitors: Structural and pharmacological perspectives
The PIM kinase, also known as serine/threonine kinase plays an important role in cancer
biology and is found in three different isoforms namely PIM-1, PIM-2, and PIM-3. They are …
biology and is found in three different isoforms namely PIM-1, PIM-2, and PIM-3. They are …
Thiazolidine-2, 4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions
Abstract Thiazolidine-2, 4-dione is an extensively explored heterocyclic nucleus for
designing of novel agents implicated for a wide variety of pathophysiological conditions, that …
designing of novel agents implicated for a wide variety of pathophysiological conditions, that …