US 20140147866A1

(19) United States

(12) Patent Application Publication (10) Pub. No.: US 2014/0147866 A1
(43) Pub. Date:

PARK et al.
(54)

COMPOUND FOR INHIBITING SNAIL-P53

BINDING AND THERAPEUTIC AGENT FOR
CANCER INCLUDING THE COMPOUND AS
EFFECTIVE COMPONENT

(22) Filed:

May 29, 2014

Dec. 31, 2013

Related US. Application Data

(62) Division of application No. 13/130,159, ?led on May

19, 2011, now abandoned, ?led as application No.

(71) Applicants:THE INDUSTRY & ACADEMIC

PCT/KR2009/006896 on Nov. 23, 2009.

COOPERATION IN CHUNGNAM

NATIONAL UNIVERSITY, Daejeon

(30)

Foreign Application Priority Data

(KR); PUSAN NATIONAL

UNIVERSITY
INDUSTRY-UNIVERSITY

COOPERATION FOUNDATION,

Pusan (KR)
(72)

Inventors: Bum Joon PARK, Busan (KR); Nam

Chul Ha, Busan (KR); Sun Hye Lee,

Busan (KR); Gyu Yong Song, Daejeon

(KR); Jee Hyun Lee, Daejeon (KR)
(73) Assignees: THE INDUSTRY & ACADEMIC
COOPERATION IN CHUNGNAM

NATIONAL UNIVERSITY, Daejeon

(KR); PUSAN NATIONAL
UNIVERSITY
INDUSTRY-UNIVERSITY

COOPERATION FOUNDATION,

Pusan (KR)

Nov. 21, 2008

(KR) ...................... .. 10-2008-0116343

Mar. 5, 2009

(KR)

10-2009-0018956

Aug. 17,2009

(KR)

10-2009-0075529

Nov. 18, 2009

(KR) ...................... .. 10-2009-0111710

Publication Classi?cation

(51)
(52)

Int. Cl.
G01N 33/574
US. Cl.

(2006.01)

CPC ................................ .. G01N33/5748 (2013.01)

USPC

....................................................... ..

435/792

(57)
ABSTRACT
Provided are compounds for inhibiting Snail-p53 binding and
therapeutic agents for cancer including the compounds as an

effective component. The Snail-p53 binding inhibitors

induce expression of p53 in K-Ras mutant cell lines, thereby
enabling effective treatment or prevention of K-Ras mutant

cancer, such as, pancreatic cancer, lung cancer, cholangioma,

(21) App1.No.: 14/144,603

and colon cancer, of Which diagnosis or treatment is not easy.

Patent Application Publication

May 29, 2014 Sheet 1 0f 23

US 2014/0147866 A1

FIG. 1

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May 29, 2014 Sheet 2 0f 23

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US 2014/0147866 A1

Patent Application Publication

May 29, 2014 Sheet 3 0f 23

US 2014/0147866 A1

FIG 3

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May 29, 2014 Sheet 5 0f 23

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May 29, 2014 Sheet 6 0f 23

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May 29, 2014 Sheet 7 0f 23

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May 29, 2014 Sheet 8 0f 23

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Patent Application Publication

May 29, 2014 Sheet 9 0f 23

US 2014/0147866 A1

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May 29, 2014 Sheet 10 0f 23

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Patent Application Publication

May 29, 2014 Sheet 11 0f 23

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Patent Application Publication

May 29, 2014 Sheet 12 0f 23

US 2014/0147866 A1

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Patent Application Publication

May 29, 2014 Sheet 13 0f 23

US 2014/0147866 A1

FIG. 13

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mm

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May 29, 2014 Sheet 14 0f 23

US 2014/0147866 A1

Ros

Patent Application Publication

May 29, 2014 Sheet 15 0f 23

US 2014/0147866 A1

Patent Application Publication

May 29, 2014 Sheet 16 0f 23

FIG. 16

US 2014/0147866 A1

Patent Application Publication

May 29, 2014 Sheet 17 0f 23

US 2014/0147866 A1

FIG 17

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Patent Application Publication

May 29, 2014 Sheet 18 0f 23

US 2014/0147866 A1

FIG. 18

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Patent Application Publication

May 29, 2014 Sheet 19 0f 23

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US 2014/0147866 A1