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Synthesis and evaluation of novel kinase inhibitors as anti-metastasis agents for

Award Number: R43CA183195
ORGANIZATION: NATIONAL CANCER INSTITUTE
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 08/01/2014
PERIOD OF PERFORMANCE END DATE: 01/31/2017

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Synthesis and evaluation of novel kinase inhibitors as anti-metastasis agents for - PROJECT SUMMARY Metastasis is a key factor for poor prognosis in cancer patients. Ovarian cancer is the fifth most common gynecological cancer causing significant mortality among women. Breast cancer is the most common invasive cancer in women and the second-most common cause of death in American women. Triple negative breast cancer tends to be both unresponsive to chemotherapy and more aggressive than other types of breast cancer. New therapies to prevent spread of these cancer types are urgently needed. There is recent scientific evidence that both migration and cytoskeleton rearrangement associated with metastases of these cancer types is controlled by a specific protein kinase. By using a rational design approach that combines structural protein kinase information and optimal ADME properties, we have discovered a novel series of potent kinase inhibitors. The goal of this work is to optimize our newly discovered series of inhibitors as agents to prevent metastasis in triple negative breast cancer and ovarian cancer. Preliminary data indicates that the lead is effective in inhibiting the migration of triple negative breast and ovarian cancer cells. In this work, new compounds will be identified utilizing our assay cascade combining in vitro receptor pharmacology and cell mobility assays to select lead molecules. Candidate ligands will be designed and synthesized using a series of recognized approaches in medicinal chemistry. Our study will open up a new avenue of target-specific drug development for specific types of breast cancer patients such as TNBC and ovarian cancer.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2017 ( Subtotal = $0 )
2017	2014	EPIGEN BIOSCIENCES INC.	10225 BARNES CANYON RD, STE A104	SAN DIEGO	CA	92121	SAN DIEGO	USA	Cancer Treatment Research	000	1	6/1/2017	NEW	$0
														Subtotal = $0

Issue Date FY: 2016 ( Subtotal = $0 )
2016	2014	EPIGEN BIOSCIENCES INC	10225 BARNES CANYON ROAD	SAN DIEGO	CA	92121	SAN DIEGO	USA	Cancer Treatment Research	000	1	1/26/2016	NEW	$0
														Subtotal = $0

Issue Date FY: 2014 ( Subtotal = $225,000 )
2014	2014	EPIGEN BIOSCIENCES INC	10225 BARNES CANYON ROAD	SAN DIEGO	CA	92121	SAN DIEGO	USA	Cancer Treatment Research	000	1	8/1/2014	NEW	$225,000
														Subtotal = $225,000

Grand Total All Awards = $225,000

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Synthesis and evaluation of novel kinase inhibitors as anti-metastasis agents for

Award Number: R43CA183195

ORGANIZATION: NATIONAL CANCER INSTITUTE

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 08/01/2014

PERIOD OF PERFORMANCE END DATE: 01/31/2017

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